Application of composition of benzimidazolyl and 2-chloroethylamino derivatives of guava dialdehyde heteroterpene in preparing anti-inflammatory drugs

A composition and drug technology, applied in the direction of drug combination, anti-inflammatory agent, medical preparations containing active ingredients, etc., can solve the problems of high toxicity and low safety

Inactive Publication Date: 2018-06-22
CHANGZHOU HIGH TECH RES INST OF NANJING UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The existing drugs for the treatment of inflammation have the problems of high toxicity and low safety. It is of great value to find compounds or lead compounds from natural products and carry out structural modification to obtain their derivatives, so as to obtain potential drugs with high efficiency and low toxicity

Method used

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  • Application of composition of benzimidazolyl and 2-chloroethylamino derivatives of guava dialdehyde heteroterpene in preparing anti-inflammatory drugs
  • Application of composition of benzimidazolyl and 2-chloroethylamino derivatives of guava dialdehyde heteroterpene in preparing anti-inflammatory drugs
  • Application of composition of benzimidazolyl and 2-chloroethylamino derivatives of guava dialdehyde heteroterpene in preparing anti-inflammatory drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] Example 1 Preparation of a guava dialdehyde heteroterpene

[0013] A preparation method of guava dialdehyde heteroterpenoids (I) refers to the literature published by Meng Shao et al. (MengShao et al., 2010. 12 (2010) 5040–5043) method.

[0014]

Embodiment 2

[0015] Example 2 Synthesis of an O-bromoethyl derivative (II) of guava dialdehyde heteroterpene

[0016] Compound I (474 ​​mg, 1.00 mmol) was dissolved in 20 mL of benzene, tetrabutylammonium bromide (TBAB) (0.16 g), 1,2-dibromoethane (7.520 g, 40.00 mmol) and 12 mL of 50% sodium hydroxide solution. The mixture was stirred at 35 °C for 8 h. After 8 hours, the reaction solution was poured into ice water, extracted twice with dichloromethane immediately, and the organic phase solutions were combined. Then the organic phase solution was washed with water and saturated brine three times successively, then dried with anhydrous sodium sulfate, and finally concentrated under reduced pressure to remove the solvent to obtain a crude product. The crude product was purified by silica gel column chromatography (mobile phase: petroleum ether / acetone=100:0.5, v / v), the brown concentrated elution band was collected and the solvent was evaporated to obtain a brown powder of Compound II (502...

Embodiment 3

[0021] Example 3 Synthesis of O-(benzimidazolyl) ethyl derivative (III) of guava dialdehyde heteroterpene

[0022] Compound II (344mg, 0.5mmol) was dissolved in 25mL of acetonitrile, anhydrous potassium carbonate (690mg, 5.0mmol), potassium iodide (168mg, 1.0mmol) and benzimidazole (4720mg, 40mmol) were added thereto, and the mixture was heated to reflux for 3h . After the reaction was completed, the reaction solution was poured into 20 mL of ice water, extracted three times with an equal amount of dichloromethane, and the organic phases were combined. The combined organic phases were successively washed with water and saturated brine, dried over anhydrous sodium sulfate, and concentrated under reduced pressure to remove the solvent to obtain a crude product. The crude product was purified by silica gel column chromatography (mobile phase: petroleum ether / acetone=100:0.5, v / v), the yellow concentrated elution band was collected and the solvent was evaporated to obtain a yello...

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PUM

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Abstract

The invention discloses an application of a composition of benzimidazolyl and 2-chloroethylamino derivatives of guava dialdehyde heteroterpene in preparing anti-inflammatory drugs, relates to the fields of organic synthesis and medicinal chemistry, and in particular relates to the composition of benzimidazolyl and 2-chloroethylamino derivatives of guava dialdehyde heteroterpene, a prepariaotn method of the composition, and the application of the composition in preparing the anti-inflammatory drugs. The invention discloses the composition of the benzimidazolyl and 2-chloroethylamino derivativesof guava dialdehyde heteroterpene and the preparation method of the composition. The pharmacological experiment shows that the composition of the benzimidazolyl and 2-chloroethylamino derivatives ofguava dialdehyde heteroterpene has the anti-inflammation effect and has the value of being developed into the anti-inflammatory drugs.

Description

technical field [0001] The invention relates to the fields of organic synthesis and medicinal chemistry, in particular to a composition, a preparation method and an application thereof. Background technique [0002] Inflammation occurs locally but can also affect the whole body. Local clinical features are redness, heat, swelling, pain and dysfunction. Redness and heat are due to the expansion of local blood vessels and the acceleration of blood flow due to inflammation. Swelling is caused by local inflammatory hyperemia and exudation of blood flow components. The development of drugs with anti-inflammatory effects is of great significance for the verification of relief and pain relief. [0003] The existing drugs for the treatment of inflammation have the problems of high toxicity and low safety. It is of great value to find compounds or lead compounds from natural products and carry out structural modification to obtain their derivatives, so as to obtain potential drugs...

Claims

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Application Information

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IPC IPC(8): A61K31/4184A61K31/335A61P29/00C07D405/14C07D313/06
CPCA61K31/335A61K31/4184C07D313/06C07D405/14A61K2300/00
Inventor 华子春李媛媛
Owner CHANGZHOU HIGH TECH RES INST OF NANJING UNIV
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